| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PROTAC ERα degrader-11 (compound W2) (96 hours) showed excellent cell inhibitory activity with IC50 values of 0.19 μM (MCF-7), 1.40 μM (MCF-7EGFR), 4.31 μM (MCF-7D538G), and 9.29 μM (MCF-7Y537S) [1]. PROTAC ERα degrader-11 (10 μM, 0-24 hours) degraded ERα in MCF-7 cells in a time-dependent manner over 24 hours, and the degradation effect was weakened after the addition of ERα ligand (OBHSA) or CRBN ligand [1]. PROTAC ERα degrader-11 (0.5-10 μM, 24 hours) did not degrade ERβ in PC9 cells [1]. PROTAC ERα degrader-11 (0-80 μM, 10-360 min) showed a concentration- and time-dependent increase in fluorescence intensity ratios [1]. PROTAC ERα degrader-11 (1-20 μM, 48 h) induced G2/M phase arrest and apoptosis in MCF-7 cells [1]. PROTAC ERα degrader-11 (10 μM, 0-60 min) showed high photostability in the presence of ERα [1]. PROTAC ERα degrader-11 (0.1-20 μM) did not cause significant damage to the blood cell membranes of SD rats [1].
|
|---|---|
| ln Vivo |
PROTAC ERα degrader-11 (compound W2) (500 mg/kg, single intraperitoneal injection) was well tolerated at doses up to 500 mg/kg and showed no acute toxicity in athymic nude mice [1].
|
| Cell Assay |
Cell cycle analysis [1]
Cell Types: MCF-7 cells Tested Concentrations: 1, 10 μM Incubation Duration: 48 hours Experimental Experimental Results: G2/M phase arrest was induced in MCF-7 cells in a dose-dependent manner. Apoptosis analysis [1] Cell Types: MCF-7 cells Tested Concentrations: 10, 20 μM Incubation Duration: 48 hours Experimental Results: Apoptosis was induced in MCF-7 cells in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models:Female BALB/c nude mice (5 weeks old) [1]
Doses: 500 mg/kg Route of Administration:Single intraperitoneal injection Experimental Results:No treatment-related death or toxic clinical signs (including piloerection, lethargy, or neurological abnormalities) were observed. No abnormal changes in body weight were observed. |
| References |
| Molecular Formula |
C51H47F3N4O12S
|
|---|---|
| Molecular Weight |
997.00
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=S(N(C1=CC=C(OCC(NCCCCCCOC2=CC3=CC=CC(C4=O)=C3C(C(N4C(C5=O)CCC(N5)=O)=O)=C2)=O)C=C1)CC(F)(F)F)([C@H]6[C@@H]7C(C8=CC=C(O)C=C8)=C(C9=CC=C(O)C=C9)[C@@H](O7)C6)=O
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0030 mL | 5.0150 mL | 10.0301 mL | |
| 5 mM | 0.2006 mL | 1.0030 mL | 2.0060 mL | |
| 10 mM | 0.1003 mL | 0.5015 mL | 1.0030 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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